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公开(公告)号：US09278944B2
公开(公告)日：2016-03-08
申请号：US14005512
申请日：2012-03-15
申请人： Toru Iijima , Hiroshi Sugama , Takayuki Kawaguchi , Jingkang Shen , Guangxin Xia , Jianshu Xie , Miki Hirai
发明人： Toru Iijima , Hiroshi Sugama , Takayuki Kawaguchi , Jingkang Shen , Guangxin Xia , Jianshu Xie , Miki Hirai
IPC分类号： C07D241/36 , C07D265/30 , C07D403/12 , C07D405/12 , C07D413/12 , C07D413/14 , C07D471/04 , C07D231/56
CPC分类号： C07D265/30 , C07D231/56 , C07D403/12 , C07D405/12 , C07D413/12 , C07D413/14 , C07D471/04
摘要： The present invention provides a nitrogen-containing saturated heterocyclic compound of the formula [I]: wherein R1 is a cycloalkyl group and the like, R22 is an optionally substituted aryl and the like, R is a lower alkyl and the like, T is a carbonyl group, Z is —O— and the like, and R3 to R6 are the same or different and a hydrogen atom and the like; or a pharmaceutically acceptable salt, that is useful as a renin inhibitor.
摘要翻译： 本发明提供式[I]的含氮饱和杂环化合物：其中R 1为环烷基等，R 22为任意取代的芳基等，R为低级烷基等，T为 羰基，Z为-O-等，R3〜R6相同或不同，为氢原子等; 或药学上可接受的盐，其可用作肾素抑制剂。
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公开(公告)号：US08975252B2
公开(公告)日：2015-03-10
申请号：US12664637
申请日：2008-06-16
申请人： Hidenori Akatsuka , Hiroshi Sugama , Nobumasa Awai , Takayuki Kawaguchi , Yoichi Takahashi , Toru Iijima , Jingkang Shen , Guangxin Xia , Jianshu Xie
发明人： Hidenori Akatsuka , Hiroshi Sugama , Nobumasa Awai , Takayuki Kawaguchi , Yoichi Takahashi , Toru Iijima , Jingkang Shen , Guangxin Xia , Jianshu Xie
IPC分类号： A61K31/535 , C07D265/30 , C07D209/08 , C07D209/14 , C07D209/30 , C07D209/34 , C07D209/42 , C07D231/56 , C07D265/36 , C07D403/04 , C07D413/04 , C07D413/12 , C07D413/14 , C07D417/14 , C07D471/04
CPC分类号： C07D265/30 , C07D209/08 , C07D209/14 , C07D209/30 , C07D209/34 , C07D209/42 , C07D231/56 , C07D265/36 , C07D403/04 , C07D413/04 , C07D413/12 , C07D413/14 , C07D417/14 , C07D471/04
摘要： The present invention provides a morpholine derivative of the formula [I]; wherein R1 is a substituted alkyl group, an optionally substituted aryl group, an optionally substituted heterocyclo group, a cycloalkyl group or an alkyl group; R2 is a substituted alkyl group, an optionally substituted aryl group, an optionally substituted heterocyclo group, an optionally substituted alkylcarbonyl group, an optionally substituted arylcarbonyl group, an optionally substituted heterocyclo-substituted carbonyl group or a cycloalkylcarbonyl group; T is a methylene group or a carbonyl group; R3, R4, R5 and R6 are the same or different and a hydrogen atom, an optionally substituted carbamoyl group or an optionally substituted alkyl group; or pharmaceutically acceptable salts thereof. These compounds are useful as a renin inhibitor.
摘要翻译： 本发明提供式[I]的吗啉衍生物。 其中R1是取代的烷基，任选取代的芳基，任选取代的杂环基，环烷基或烷基; R 2是取代的烷基，任选取代的芳基，任选取代的杂环基，任选取代的烷基羰基，任选取代的芳基羰基，任选取代的杂环取代的羰基或环烷基羰基; T是亚甲基或羰基; R3，R4，R5和R6相同或不同，氢原子，任选取代的氨基甲酰基或任选取代的烷基; 或其药学上可接受的盐。 这些化合物可用作肾素抑制剂。
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公开(公告)号：US20100240644A1
公开(公告)日：2010-09-23
申请号：US12664637
申请日：2008-06-16
申请人： Hidenori Akatsuka , Hiroshi Sugama , Nobumasa Awai , Takayuki Kawaguchi , Yoichi Takahashi , Toru Iijima , Jingkang Shen , Guangxin Xia , Jianshu Xie
发明人： Hidenori Akatsuka , Hiroshi Sugama , Nobumasa Awai , Takayuki Kawaguchi , Yoichi Takahashi , Toru Iijima , Jingkang Shen , Guangxin Xia , Jianshu Xie
IPC分类号： A61K31/538 , C07D265/30 , A61K31/5375 , C07D265/36 , C07D413/12 , A61K31/5377 , C07D409/12 , A61K31/5355 , A61P9/12
CPC分类号： C07D265/30 , C07D209/08 , C07D209/14 , C07D209/30 , C07D209/34 , C07D209/42 , C07D231/56 , C07D265/36 , C07D403/04 , C07D413/04 , C07D413/12 , C07D413/14 , C07D417/14 , C07D471/04
摘要： The present invention provides a morpholine derivative of the formula [I]; wherein R1 is a substituted alkyl group, an optionally substituted aryl group, an optionally substituted heterocyclo group, a cycloalkyl group or an alkyl group; R2 is a substituted alkyl group, an optionally substituted aryl group, an optionally substituted heterocyclo group, an optionally substituted alkylcarbonyl group, an optionally substituted arylcarbonyl group, an optionally substituted heterocyclo-substituted carbonyl group or a cycloalkylcarbonyl group; T is a methylene group or a carbonyl group; R3, R4, R5 and R6 are the same or different and a hydrogen atom, an optionally substituted carbamoyl group or an optionally substituted alkyl group; or pharmaceutically acceptable salts thereof. These compounds are useful as a renin inhibitor.
摘要翻译： 本发明提供式[I]的吗啉衍生物。 其中R1是取代的烷基，任选取代的芳基，任选取代的杂环基，环烷基或烷基; R 2是取代的烷基，任选取代的芳基，任选取代的杂环基，任选取代的烷基羰基，任选取代的芳基羰基，任选取代的杂环取代的羰基或环烷基羰基; T是亚甲基或羰基; R3，R4，R5和R6相同或不同，氢原子，任选取代的氨基甲酰基或任选取代的烷基; 或其药学上可接受的盐。 这些化合物可用作肾素抑制剂。
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公开(公告)号：US20140011807A1
公开(公告)日：2014-01-09
申请号：US14005512
申请日：2012-03-15
申请人： Toru Iijima , Hiroshi Sugama , Takayuki Kawaguchi , Jingkang Shen , Guangxin Xia , Jianshu Xie
发明人： Toru Iijima , Hiroshi Sugama , Takayuki Kawaguchi , Jingkang Shen , Guangxin Xia , Jianshu Xie
IPC分类号： C07D265/30 , C07D403/12 , C07D231/56 , C07D413/14 , C07D405/12 , C07D413/12 , C07D471/04
CPC分类号： C07D265/30 , C07D231/56 , C07D403/12 , C07D405/12 , C07D413/12 , C07D413/14 , C07D471/04
摘要： The present invention provides a nitrogen-containing saturated heterocyclic compound of the formula [I]: wherein R1 is a cycloalkyl group and the like, R22 is an optionally substituted aryl and the like, R is a lower alkyl and the like, T is a carbonyl group, Z is —O— and the like, and R3 to R6 are the same or different and a hydrogen atom and the like; or a pharmaceutically acceptable salt, that is useful as a renin inhibitor.
摘要翻译： 本发明提供式[I]的含氮饱和杂环化合物：其中R 1为环烷基等，R 22为任意取代的芳基等，R为低级烷基等，T为 羰基，Z为-O-等，R3〜R6相同或不同，为氢原子等; 或药学上可接受的盐，其可用作肾素抑制剂。
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公开(公告)号：US07514439B2
公开(公告)日：2009-04-07
申请号：US11660905
申请日：2006-07-10
IPC分类号： A61K31/341 , A61K31/427 , A61K31/4525 , A61K31/496 , C07D307/20 , C07D277/44 , C07D405/14 , C07D417/14
CPC分类号： C07D405/12 , A61K31/433 , C07D213/75 , C07D241/20 , C07D277/46 , C07D285/01 , C07D403/06 , C07D405/14 , C07D417/12 , C07D417/14 , C07D513/04
摘要： The problem of the present invention is to provide a useful compound as a glucokinase activating agent, which is the oxime derivative of the formula [I]: wherein Ring A is aryl or heteroaryl; Q is cycloalkyl, heterocycle, alkyl or alkenyl; Ring T is heteroaryl or heterocycle; R1 and R2 are independently hydrogen atom, halogen atom, cycloalkylsulfonyl or the like; R3 and R4 are independently hydrogen atom, hydroxy, oxo, halogen atom or the like; R5 is hydrogen atom, halogen atom, cyano, nitro, tetrazolyl or the like; or a pharmaceutically acceptable salt thereof.
摘要翻译： 本发明的问题是提供作为葡糖激酶活化剂的有用化合物，其为式[I]的肟衍生物：其中环A为芳基或杂芳基; Q是环烷基，杂环，烷基或烯基; 环T是杂芳基或杂环; R1和R2独立地为氢原子，卤素原子，环烷基磺酰基等; R3和R4独立地是氢原子，羟基，氧代，卤素原子等; R5是氢原子，卤素原子，氰基，硝基，四唑基等; 或其药学上可接受的盐。
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公开(公告)号：US20100099662A1
公开(公告)日：2010-04-22
申请号：US12522663
申请日：2008-01-09
IPC分类号： A61K31/553 , A61K31/55 , A61K31/551 , A61K31/541 , A61K31/5377 , A61K31/496 , A61K31/437 , A61K31/4439 , A61K31/433 , A61K31/427 , C07D417/14 , C07D417/12 , C07D403/12 , C07D513/04 , C07D401/12 , C07D277/38 , A61P3/04 , A61P3/10 , A61P27/02 , A61P25/00
CPC分类号： C07D213/75 , C07D213/80 , C07D239/42 , C07D239/72 , C07D241/20 , C07D261/14 , C07D277/20 , C07D277/46 , C07D277/56 , C07D285/08 , C07D285/135 , C07D417/06 , C07D417/12 , C07D417/14 , C07D487/08 , C07D498/04 , C07D513/04
摘要： A hydrazone derivative of formula [I]: wherein Ring A is aryl or heteroaryl, Ring T is heteroaryl or heterocycle, R1 and R2 are independently hydrogen atom, halogen atom, cycloalkylsulfonyl, etc., R3 and R4 combine each other together with the adjacent nitrogen atom to form substituted or unsubstituted heterocycle, R5 is hydrogen atom, halogen atom, cyano, nitro, tetrazolyl, etc., and R6 is hydrogen atom, etc.;or a pharmaceutically acceptable salt thereof is useful as a glucokinase activation agent.
摘要翻译： 式[I]的腙衍生物：其中环A是芳基或杂芳基，环T是杂芳基或杂环，R 1和R 2独立地是氢原子，卤素原子，环烷基磺酰基等，R 3和R 4彼此结合， 氮原子以形成取代或未取代的杂环，R5为氢原子，卤原子，氰基，硝基，四唑基等，R6为氢原子等。 或其药学上可接受的盐可用作葡糖激酶活化剂。
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公开(公告)号：US08314247B2
公开(公告)日：2012-11-20
申请号：US12522663
申请日：2008-01-09
IPC分类号： A61K31/427 , C07D417/12 , C07D417/14
CPC分类号： C07D213/75 , C07D213/80 , C07D239/42 , C07D239/72 , C07D241/20 , C07D261/14 , C07D277/20 , C07D277/46 , C07D277/56 , C07D285/08 , C07D285/135 , C07D417/06 , C07D417/12 , C07D417/14 , C07D487/08 , C07D498/04 , C07D513/04
摘要： A hydrazone derivative of formula [I]: wherein Ring A is aryl or heteroaryl, Ring T is heteroaryl or heterocycle, R1 and R2 are independently hydrogen atom, halogen atom, cycloalkylsulfonyl, etc., R3 and R4 combine each other together with the adjacent nitrogen atom to form substituted or unsubstituted heterocycle, R5 is hydrogen atom, halogen atom, cyano, nitro, tetrazolyl, etc., and R6 is hydrogen atom, etc.; or a pharmaceutically acceptable salt thereof is useful as a glucokinase activation agent.
摘要翻译： 式[I]的腙衍生物：其中环A是芳基或杂芳基，环T是杂芳基或杂环，R 1和R 2独立地是氢原子，卤素原子，环烷基磺酰基等，R 3和R 4彼此结合， 氮原子以形成取代或未取代的杂环，R5为氢原子，卤原子，氰基，硝基，四唑基等，R6为氢原子等。 或其药学上可接受的盐可用作葡糖激酶活化剂。
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公开(公告)号：US20080132479A1
公开(公告)日：2008-06-05
申请号：US11660905
申请日：2006-07-10
IPC分类号： A61K31/427 , A61P3/10 , A61P25/00 , A61P9/10 , A61P3/04 , C07D417/14 , C07D487/02 , A61K31/551 , A61K31/454 , A61K31/433 , C07D417/02 , A61K31/4985 , A61K31/496 , A61K31/437 , C07D513/04 , A61K31/541 , A61K31/5377
CPC分类号： C07D405/12 , A61K31/433 , C07D213/75 , C07D241/20 , C07D277/46 , C07D285/01 , C07D403/06 , C07D405/14 , C07D417/12 , C07D417/14 , C07D513/04
摘要： The problem of the present invention is to provide a useful compound as a glucokinase activating agent, which is the oxime derivative of the formula [I]: wherein Ring A is aryl or heteroaryl; Q is cycloalkyl, heterocycle, alkyl or alkenyl; Ring T is heteroaryl or heterocycle; R1 and R2 are independently hydrogen atom, halogen atom, cycloalkylsulfonyl or the like; R3 and R4 are independently hydrogen atom, hydroxy, oxo, halogen atom or the like; R5 is hydrogen atom, halogen atom, cyano, nitro, tetrazolyl or the like; or a pharmaceutically acceptable salt thereof.
摘要翻译： 本发明的问题是提供作为葡糖激酶活化剂的有用化合物，其为式[I]的肟衍生物：其中环A为芳基或杂芳基; Q是环烷基，杂环，烷基或烯基; 环T是杂芳基或杂环; R 1和R 2独立地是氢原子，卤素原子，环烷基磺酰基等; R 3和R 4独立地是氢原子，羟基，氧代，卤素原子等; R 5是氢原子，卤素原子，氰基，硝基，四唑基等; 或其药学上可接受的盐。
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公开(公告)号：US08119626B2
公开(公告)日：2012-02-21
申请号：US12274674
申请日：2008-11-20
IPC分类号： A61K31/427 , A61K31/496 , A61K31/497 , C07D417/12 , C07D413/14 , C07D405/12
CPC分类号： C07D405/12 , A61K31/433 , C07D213/75 , C07D241/20 , C07D277/46 , C07D285/01 , C07D403/06 , C07D405/14 , C07D417/12 , C07D417/14 , C07D513/04
摘要： The problem of the present invention is to provide a useful compound as a glucokinase activating agent, which is the oxime derivative of the formula [I]: wherein Ring A is aryl or heteroaryl; Q is cycloalkyl, heterocycle, alkyl or alkenyl; Ring T is heteroaryl or heterocycle; R1 and R2 are independently hydrogen atom, halogen atom, cycloalkylsulfonyl or the like; R3 and R4 are independently hydrogen atom, hydroxy, oxo, halogen atom or the like; R5 is hydrogen atom, halogen atom, cyano, nitro, tetrazolyl or the like; or a pharmaceutically acceptable salt thereof.
摘要翻译： 本发明的问题是提供作为葡糖激酶活化剂的有用化合物，其为式[I]的肟衍生物：其中环A为芳基或杂芳基; Q是环烷基，杂环，烷基或烯基; 环T是杂芳基或杂环; R1和R2独立地为氢原子，卤素原子，环烷基磺酰基等; R3和R4独立地是氢原子，羟基，氧代，卤素原子等; R5是氢原子，卤素原子，氰基，硝基，四唑基等; 或其药学上可接受的盐。
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公开(公告)号：US20090291936A1
公开(公告)日：2009-11-26
申请号：US12274674
申请日：2008-11-20
IPC分类号： A61K31/427 , C07D417/12 , A61K31/496 , C07D413/14 , A61K31/497 , C07D405/12
CPC分类号： C07D405/12 , A61K31/433 , C07D213/75 , C07D241/20 , C07D277/46 , C07D285/01 , C07D403/06 , C07D405/14 , C07D417/12 , C07D417/14 , C07D513/04
摘要： The problem of the present invention is to provide a useful compound as a glucokinase activating agent, which is the oxime derivative of the formula [I]: wherein Ring A is aryl or heteroaryl; Q is cycloalkyl, heterocycle, alkyl or alkenyl; Ring T is heteroaryl or heterocycle; R1 and R2 are independently hydrogen atom, halogen atom, cycloalkylsulfonyl or the like; R3 and R4 are independently hydrogen atom, hydroxy, oxo, halogen atom or the like; R5 is hydrogen atom, halogen atom, cyano, nitro, tetrazolyl or the like; or a pharmaceutically acceptable salt thereof.
摘要翻译： 本发明的问题是提供作为葡糖激酶活化剂的有用化合物，其为式[I]的肟衍生物：其中环A为芳基或杂芳基; Q是环烷基，杂环，烷基或烯基; 环T是杂芳基或杂环; R1和R2独立地为氢原子，卤素原子，环烷基磺酰基等; R3和R4独立地是氢原子，羟基，氧代，卤素原子等; R5是氢原子，卤素原子，氰基，硝基，四唑基等; 或其药学上可接受的盐。
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